[Binding of a tetrabenazine derivative to the monoamine transporter of the chromaffin granule membrane].
[2-3H] dihydrotetrabenazine (2-hydroxy-3-isobutyl-9-10-dimethoxy-1,2,3,4,6,7 hexahydro-11 bH-benzo [a] quinolizine), a derivative of tetrabenazine obtained by tritiated borohydride reduction, binds to the membrane of purified chromaffin granules. The binding equilibrium has been studied by filtration and by centrifugation of ligand-membrane complexes. Saturable binding sites (190 pmol/mg protein), characterized by a dissociation equilibrium constant KD = 90 nM have been described. The correlation existing between dihydrotetrabenazine site occupancy and noradrenaline uptake inhibition indicates that these sites are located on the monoamine transporter.
D000255:Adenosine Triphosphate / Q000378:metabolism; D001665:Binding Sites; D001679:Biogenic Amines / Q000378:metabolism*; D001693:Biological Transport, Active / Q000187:drug effects; D002837:Chromaffin Granules / Q000378:metabolism*; D002838:Chromaffin System / Q000378:metabolism*; D066298:In Vitro Techniques; D008566:Membranes / Q000378:metabolism; D009638:Norepinephrine / Q000378:metabolism; D013747:Tetrabenazine / Q000031:analogs & derivatives* / Q000378:metabolism
D001679:Biogenic Amines; C032811:dihydrotetrabenazine; D000255:Adenosine Triphosphate; D009638:Norepinephrine; D013747:Tetrabenazine
Liaison d'un dérivé de la tétrabénazine au transporteur des monoamines de la membrane des granules chromaffines.